Pub. Date : 2016 Jul 1
PMID : 27060207
7 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | Cabozantinib is selectively cytotoxic in acute myeloid leukemia cells with FLT3-internal tandem duplication (FLT3-ITD). | cabozantinib | fms related receptor tyrosine kinase 3 | Homo sapiens |
| 2 | Cabozantinib is selectively cytotoxic in acute myeloid leukemia cells with FLT3-internal tandem duplication (FLT3-ITD). | cabozantinib | fms related receptor tyrosine kinase 3 | Homo sapiens |
| 3 | We found that cabozantinib was significantly cytotoxic to MV4-11 and Molm-13 cells that harbored FLT3-ITD, resulting in IC50 values of 2.4 nM and 2.0 nM, respectively. | cabozantinib | fms related receptor tyrosine kinase 3 | Homo sapiens |
| 4 | However, K562, OCI-AML3 and THP-1 (leukemia cell lines lacking FLT3-ITD) were resistant to cabozantinib, showing IC50 values in the micromolar range. | cabozantinib | fms related receptor tyrosine kinase 3 | Homo sapiens |
| 5 | Cabozantinib arrested MV4-11 cell growth at the G0/G1 phase within 24 h, which was associated with decreased phosphorylation of FLT3, STAT5, AKT and ERK. | cabozantinib | fms related receptor tyrosine kinase 3 | Homo sapiens |
| 6 | Thus, cabozantinib is selectively cytotoxic to leukemia cells with FLT3-ITD, causing cell-cycle arrest and apoptosis. | cabozantinib | fms related receptor tyrosine kinase 3 | Homo sapiens |
| 7 | Clinical trials evaluating the efficacy of cabozantinib in acute myeloid leukemia (AML) with FLT3-ITD are warranted. | cabozantinib | fms related receptor tyrosine kinase 3 | Homo sapiens |